Metabolism of Beclamide, N-Benzyl-3-chloropropionamide, in Man

Abstract

1. Following oral administration of [¹⁴C]beclamide to human subjects there was almost complete elimination of radioactivity in the urine within 48 h.

2. Less than 1% of the administered dose was excreted unchanged.

3. The major metabolites were (a) N-(4-hydroxybenzyl)-3-chloropropionamide, (4-hydroxybeclamide; c. 56%), which was eliminated to a small extent in the free form and as a sulphate but mainly as a glucuronide, and (b) hippuric acid (c. 20%).

4. Six minor metabolites were also detected, of which the following were identified: benzoic acid (up to c. 7%), N-(4-hydroxybenzyl-3-chloro-2-hydroxypropionamide, (dihydroxy-beclamide; c. 2% mostly as a glucuromde) and 4-hydroxybenzoic acid (c. 0·6%, partly as a glucuronide).